公开(公告)号：US4156728A

公开(公告)日：1979-05-29

申请号：US865213

申请日：1977-12-28

申请人： Takemi Koeda ,  Takashi Tsuruoka ,  Hiroyasu Asaoka ,  Uichi Shibata ,  Shigeharu Inoue ,  Taro Niida

发明人： Takemi Koeda ,  Takashi Tsuruoka ,  Hiroyasu Asaoka ,  Uichi Shibata ,  Shigeharu Inoue ,  Taro Niida

IPC分类号： C07D213/79 ,  A61K31/44

CPC分类号： C07D213/79

摘要： Novel compounds useful as hypotensive agents are presented having the general formula I ##STR1## wherein R.sub.1 represents a substituted or unsubstituted aralkyl group, that is an aralkyl group of the general formula ##STR2## wherein R.sub.2 represents hydrogen, a lower alkyl group or a halogen atom. Furthermore, new therapeutic compositions of matter are also described incorporating the above novel 3-substituted-2(1H)pyridone-6-carboxylic acids (I) as an active ingredient with carriers and showing uses as hypotensive agents. These new compounds of the formula I are prepared by reacting D-glucaro-.delta.-lactam or its salt with an aralkyl halide.

摘要翻译： 提供了用作降压剂的新型化合物，其具有通式I（I），其中R 1表示取代或未取代的芳烷基，即通式为“IMAGE”的芳烷基，其中R 2表示氢，低级烷基 或卤素原子。 此外，还描述了新型的物质治疗组合物，其结合上述新型3-取代-2（1H）吡啶酮-6-羧酸（I）作为活性成分与载体并用作降压剂。 这些新的式I化合物通过D-葡聚糖-δ-内酰胺或其盐与芳烷基卤化物反应来制备。

公开(公告)号：US4083850A

公开(公告)日：1978-04-11

申请号：US700340

申请日：1976-06-28

申请人： Takemi Koeda ,  Takashi Tsuruoka ,  Hiroyasu Asaoka ,  Uichi Shibata ,  Shigeharu Inoue ,  Taro Niida

发明人： Takemi Koeda ,  Takashi Tsuruoka ,  Hiroyasu Asaoka ,  Uichi Shibata ,  Shigeharu Inoue ,  Taro Niida

IPC分类号： C07D213/79 ,  C07D213/55

CPC分类号： C07D213/79

摘要： Novel compounds useful as hypotensive agents are presented having the general formula I ##STR1## wherein R.sub.1 represents a lower aliphatic acyl group, a straight or branched chain alkyl or alkenyl group or an aralkyl group of the general formula ##STR2## wherein R.sub.2 represents hydrogen, a lower alkyl group or a halogen atom. Furthermore, new therapeutic compositions of matter are also described incorporating the above novel 3-substituted-2(1H)pyridone-6-carboxylic acids (I) as an active ingredient with carriers and showing uses as hypotensive agents. These new compounds of the formula I are prepared either by reacting D-glucaro-.delta.-lactam or its salt with an acid anhydride or by reacting 3-hydroxy-2(1H)pyridone-6-carboxylic acid with an acyl anhydride or alkyl halide, aralkyl halide and an alkenyl halide.

摘要翻译： 提供了可用作降压剂的新型化合物，其具有通式I（I），其中R 1表示低级脂族酰基，直链或支链烷基或烯基或通式为“IMAGE”的芳烷基，其中R 2 表示氢，低级烷基或卤素原子。 此外，还描述了新型的物质治疗组合物，其结合上述新型3-取代-2（1H）吡啶酮-6-羧酸（I）作为活性成分与载体并用作降压剂。 式I的这些新化合物通过D-葡聚糖-δ-内酰胺或其盐与酸酐反应或通过使3-羟基-2（1H）吡啶酮-6-羧酸与酰基酸酐或烷基卤化物 芳烷基卤化物和烯基卤化物。

公开(公告)号：US4198416A

公开(公告)日：1980-04-15

申请号：US944683

申请日：1978-09-22

申请人： Takemi Koeda ,  Takashi Tsuruoka ,  Uichi Shibata ,  Hiroyasu Asaoka ,  Mitsugu Hachisu ,  Osamu Itoh ,  Yasuharu Sekizawa ,  Shigeharu Inouye ,  Taro Niida

发明人： Takemi Koeda ,  Takashi Tsuruoka ,  Uichi Shibata ,  Hiroyasu Asaoka ,  Mitsugu Hachisu ,  Osamu Itoh ,  Yasuharu Sekizawa ,  Shigeharu Inouye ,  Taro Niida

IPC分类号： C07D213/65 ,  C07D213/79 ,  A61K31/44

CPC分类号： C07D213/79 ,  C07D213/65

摘要： 5-Alkoxy-picolinic esters represented by the formula (I): ##STR1## wherein R represents an alkyl group having 1 to 6 carbon atoms and R.sub.1 represents an unsubstituted phenyl group; a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms or an acetyl group; a phthalidyl group; an alkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; an alkoxyalkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; an indanyl group; or an acyloxyalkyl group having the formula ##STR2## wherein R.sub.2 represents a hydrogen atom or a methyl group and R.sub.3 represents an alkyl group having 1 to 5 carbon atoms (such as a methyl, n-propyl, isobutyl, t-butyl, etc., group), an alkoxy group having 1 to 4 carbon atoms, a phenyl group, a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as chlorine, bromine, iodine, etc., atom) or an aralkyl group wherein the alkyl moiety has 1 to 3 carbon atoms, which are useful as anti-hypertensive agents, a process for preparing 5-alkoxy-picolinic esters, and anti-hypertensive compositions containing the 5-alkoxy-picolinic esters.

摘要翻译： 由式（I）表示的5-烷氧基 - 吡啶甲酸酯：其中R表示具有1至6个碳原子的烷基，R 1表示未取代的苯基; 被一个或多个具有1至4个碳原子的烷基或乙酰基取代的苯基; 苯酞基; 其中烷基部分和烷氧基部分各自具有1至4个碳原子的烷氧基烷基; 其中烷基部分和烷氧基部分各自具有1至4个碳原子的烷氧基烷氧基烷基; 茚满基; 或具有式“IMAGE”的酰氧基烷基，其中R 2表示氢原子或甲基，R 3表示具有1至5个碳原子的烷基（例如甲基，正丙基，异丁基，叔丁基等） ，基团），具有1至4个碳原子的烷氧基，苯基，被一个或多个具有1至4个碳原子的烷基取代的苯基，具有1至4个碳原子的烷氧基或卤素原子 （例如氯，溴，碘等原子）或其中烷基部分具有1〜3个碳原子的芳烷基，其可用作抗高血压剂，制备5-烷氧基 - 吡啶甲酸酯的方法和 含有5-烷氧基 - 吡啶甲酸酯的抗高血压组合物。

公开(公告)号：US4189489A

公开(公告)日：1980-02-19

申请号：US838180

申请日：1977-09-30

申请人： Takemi Koeda ,  Takashi Tsuruoka ,  Uichi Shibata ,  Hiroyasu Asaoka ,  Mitsugu Hachisu ,  Osamu Itoh ,  Yasuharu Sekizawa ,  Shigeharu Inouye ,  Taro Niida

发明人： Takemi Koeda ,  Takashi Tsuruoka ,  Uichi Shibata ,  Hiroyasu Asaoka ,  Mitsugu Hachisu ,  Osamu Itoh ,  Yasuharu Sekizawa ,  Shigeharu Inouye ,  Taro Niida

IPC分类号： A61K31/44 ,  A61P9/12 ,  C07D213/65 ,  C07D213/79 ,  A61K31/445 ,  C07D213/89

CPC分类号： C07D213/79 ,  C07D213/65

摘要： 5-Alkoxy-picolinic acids and the salts and the esters thereof represented by the formula (I): ##STR1## wherein R represents an alkyl group having 1 to 6 carbon atoms and M represents a hydrogen atom; a calcium atom; a sodium atom; a potassium atom; an aluminum atom; an unsubstituted phenyl group; a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as a chlorine, bromine, iodine, etc., atom); a phthalidyl group; an alkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; or an acyloxyalkyl group having the formula ##STR2## wherein R.sub.2 represents a hydrogen atom or a methyl group and R.sub.3 represents an alkyl group having 1 to 5 carbon atoms (such as a methyl, n-propyl, isobutyl, t-butyl, etc., group), an alkoxy group having 1 to 4 carbon atoms, a phenyl group, a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as a chlorine, bromine, iodine, etc., atom) or an aralkyl group wherein the alkyl moiety has 1 to 3 carbon atoms, which are useful as anti-hypertensive agents, a process for preparing 5-alkoxy-picolinic acids and the salts and the esters thereof, and anti-hypertensive compositions containing the 5-alkoxy-picolinic acids and the salts and the esters thereof.

摘要翻译： 5-烷氧基 - 吡啶甲酸及其由式（I）表示的盐及其酯：其中R表示具有1至6个碳原子的烷基，M表示氢原子; 钙原子; 一个钠原子; 钾原子; 铝原子; 未取代的苯基; 被一个或多个具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基或卤素原子（例如氯，溴，碘等）原子取代的苯基; 苯酞基; 其中烷基部分和烷氧基部分各自具有1至4个碳原子的烷氧基烷基; 或具有式“IMAGE”的酰氧基烷基，其中R 2表示氢原子或甲基，R 3表示具有1至5个碳原子的烷基（例如甲基，正丙基，异丁基，叔丁基等） ，基团），具有1至4个碳原子的烷氧基，苯基，被一个或多个具有1至4个碳原子的烷基取代的苯基，具有1至4个碳原子的烷氧基或卤素原子 （例如氯，溴，碘等原子）或其中烷基部分具有1至3个碳原子的芳烷基，其可用作抗高血压剂，制备5-烷氧基 - 吡啶甲酸的方法和 其盐和酯，以及含有5-烷氧基 - 吡啶甲酸及其盐及其酯的抗高血压组合物。

公开(公告)号：US4229448A

公开(公告)日：1980-10-21

申请号：US23504

申请日：1979-03-23

申请人： Yasuharu Sekizawa ,  Takashi Tsuruoka ,  Mitsugu Hachisu ,  Masaji Sezaki ,  Masashi Miyamoto ,  Uichi Shibata ,  Kazuko Mizutani ,  Shigeharu Inouye ,  Takemi Koeda ,  Keizo Shimomura ,  Taro Niida

发明人： Yasuharu Sekizawa ,  Takashi Tsuruoka ,  Mitsugu Hachisu ,  Masaji Sezaki ,  Masashi Miyamoto ,  Uichi Shibata ,  Kazuko Mizutani ,  Shigeharu Inouye ,  Takemi Koeda ,  Keizo Shimomura ,  Taro Niida

IPC分类号： C07D213/65 ,  C07D213/79 ,  C07D213/81 ,  A61K31/455

CPC分类号： C07D213/79 ,  C07D213/65 ,  C07D213/81

摘要： 5-Substituted picolinic acid derivatives represented by the formula (I): ##STR1## wherein R.sub.1 represents a straight or branched chain halogen-substituted alkyl group having 2 to 6 carbon atoms or a substituted phenyl group having the formula ##STR2## wherein R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, an amino group, an N-alkyl-substituted amino group, an acylamino group, an acetyl group, an acyloxy group, a hydroxy group or a halogen-substituted alkyl group or R.sub.3 and R.sub.4, when taken together, represent a polymethylene chain; and R.sub.2 represents an --OM group wherein M represents a hydrogen, sodium, potassium, calcium, aluminium or magnesium atom, a straight or branched chain or cyclic alkoxy group having 1 to 6 carbon atoms, an aminoalkoxy group, a phenoxy group, a substituted phenoxy group, a 5-indanyloxy group, an acyloxyalkyloxy group having the formula ##STR3## wherein R.sub.5 represents a hydrogen atom or a methyl group and R.sub.6 represents a lower alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group, or an amino group represented by the formula ##STR4## wherein R.sub.7 and R.sub.8, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a phenyl group which are useful as anti-hypertensive agents, a process for preparing the above 5-substituted picolinic acid derivatives, and anti-hypertensive compositions containing the same.

摘要翻译： 由式（I）表示的5-取代的吡啶甲酸衍生物：其中R 1表示具有2至6个碳原子的直链或支链卤素取代的烷基或具有下式的取代苯基： 其中可以相同或不同的R 3和R 4各自表示氢原子，卤素原子，低级烷基，低级烷氧基，硝基，氨基，N-烷基取代的氨基， 酰氨基，乙酰基，酰氧基，羟基或卤素取代的烷基，或者R 3和R 4一起表示聚亚甲基链; R 2表示-OM基，其中M表示氢，钠，钾，钙，铝或镁原子，具有1至6个碳原子的直链或支链或环状烷氧基，氨基烷氧基，苯氧基，取代的 苯氧基，5-茚满氧基，具有式“IMAGE”的酰氧基烷氧基，其中R5表示氢原子或甲基，R6表示碳原子数1〜6的低级烷基，苯基或取代苯基 或由式“IMAGE”表示的氨基，其中R7和R8可以相同或不同，表示可用作抗高血压剂的氢原子，低级烷基或苯基， 制备上述5-取代的吡啶甲酸衍生物的方法和含有它们的抗高血压组合物。

公开(公告)号：US4122171A

公开(公告)日：1978-10-24

申请号：US786468

申请日：1977-04-11

申请人： Tetsutaro Niizato ,  Takashi Tsuruoka ,  Shigeharu Inouye ,  Takemi Koeda ,  Taro Niida

发明人： Tetsutaro Niizato ,  Takashi Tsuruoka ,  Shigeharu Inouye ,  Takemi Koeda ,  Taro Niida

IPC分类号： C07D211/78 ,  A61K31/445 ,  A61K31/455 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P13/02 ,  A61P15/00 ,  A61P31/04 ,  C07H15/22 ,  A61K31/71

CPC分类号： A61K31/70 ,  A61K31/445

摘要： D-glucaro-1,5-lactam and its pharmaceutically acceptable salts are useful as an agent of protecting against renal failure or damage induced by administration of aminoglycosidic antibiotics.

摘要翻译： D-葡聚糖-1,5-内酰胺及其药学上可接受的盐可用作防止肾衰竭或通过施用氨基糖苷类抗生素诱导的损伤的药剂。

公开(公告)号：US4169140A

公开(公告)日：1979-09-25

申请号：US736143

申请日：1976-10-27

申请人： Kazunori Ohba ,  Takashi Shomura ,  Hiroshi Watanabe ,  Kunikazu Totsukawa ,  Michio Kojima ,  Shoji Omoto ,  Takashi Tsuruoka ,  Shigeharu Inoue ,  Taro Niida

发明人： Kazunori Ohba ,  Takashi Shomura ,  Hiroshi Watanabe ,  Kunikazu Totsukawa ,  Michio Kojima ,  Shoji Omoto ,  Takashi Tsuruoka ,  Shigeharu Inoue ,  Taro Niida

IPC分类号： A61K35/74 ,  A61P31/04 ,  C07G11/00 ,  C12P1/06 ,  C12R1/465 ,  A61K35/00

CPC分类号： C12P1/06

摘要： A new antibiotic SF-1771 substance is produced by cultivating a new strain, Streptomyces toyocaensis SF-1771, in a liquid culture medium under aerobic conditions. This antibiotic may be isolated from the fermentation broth by treating the broth filtrate with a synthetic adsorbent resin for adsorption of the active compound and eluting the resin with an aqueous alcohol or aqueous acetone, followed by chromatographic purification. SF-1771 substance is a copper-containing antibiotic which shows antibacterial activity against Escherichia coli, Salmonella typhi, Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus subtilis. Removal of the copper component from SF-1771 substance by treatment with hydrogen sulfide, an alkali metal sulfide or a copper-chelating agent gives SF-1771-B substance containing no copper component which shows antibacterial activity as high as but a toxicity lower than SF-1771 substance.

摘要翻译： 通过在有氧条件下在液体培养基中培养新的菌株Streptomyces toyocaensis SF-1771来生产新的抗生素SF-1771物质。 通过用合成吸附剂树脂处理肉汤滤液以吸附活性化合物并用含水醇或丙酮水溶液洗脱树脂，然后进行色谱纯化，从发酵液中分离出该抗生素。 SF-1771物质是对大肠杆菌，伤寒沙门氏菌，铜绿假单胞菌，金黄色葡萄球菌和枯草芽孢杆菌具有抗菌活性的含铜抗生素。 通过用硫化氢，碱金属硫化物或铜螯合剂处理从SF-1771物质中除去铜成分得到不含铜成分的SF-1771-B物质，其抗菌活性高于但低于SF的毒性 -1771物质。

公开(公告)号：US4103083A

公开(公告)日：1978-07-25

申请号：US751877

申请日：1976-12-17

申请人： Yasuaki Ogawa ,  Yasumitsu Kondo ,  Takashi Shomura ,  Takashi Tsuruoka ,  Shigeharu Inouye ,  Taro Niida

发明人： Yasuaki Ogawa ,  Yasumitsu Kondo ,  Takashi Shomura ,  Takashi Tsuruoka ,  Shigeharu Inouye ,  Taro Niida

IPC分类号： C07D501/20 ,  C07D501/57

CPC分类号： C07D501/57 ,  Y10S435/886

摘要： Novel antibiotics derivatives 7-(5-acylamido-5-carboxyvaleramido)-3-(.alpha.-methoxy-p-acyloxycinnamoyloxymethyl)-7-methoxy-3-cephem-4-carboxylic acids and the salts thereof which are useful as antibiotics and intermediates for the preparation of cephamycin derivatives, a process for preparing the same, and a process for recovering the cephamycin derivatives effectively and stably from the fermentation broth in the form of an N-acyl derivative.

摘要翻译： 新型抗生素衍生物7-（5-酰氨基-5-羧基戊酰氨基）-3-（α-甲氧基 - 对酰氧基肉桂酰氧基甲基）-7-甲氧基-3-头孢烯-4-羧酸及其盐，可用作抗生素和中间体 用于制备头孢霉素衍生物，其制备方法，以及以N-酰基衍生物的形式从发酵液中有效稳定地回收头孢霉素衍生物的方法。

公开(公告)号：US4258184A

公开(公告)日：1981-03-24

申请号：US020224

申请日：1979-03-13

申请人： Fumio Kai ,  Takashi Tsuruoka ,  Osamu Makabe ,  Shigeharu Inouye ,  Hitoshi Ikeda ,  Yuzo Kazuno ,  Shokichi Nakajima ,  Shigeo Seki ,  Taro Niida

发明人： Fumio Kai ,  Takashi Tsuruoka ,  Osamu Makabe ,  Shigeharu Inouye ,  Hitoshi Ikeda ,  Yuzo Kazuno ,  Shokichi Nakajima ,  Shigeo Seki ,  Taro Niida

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/36 ,  C07D501/56

CPC分类号： C07D501/36 ,  A61K31/545

摘要： Novel cephalosporin derivatives having formulae (V) and (III): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.8 and A are defined as in the specification.

摘要翻译： 具有式（V）和（III）的新型头孢菌素衍生物：其中R 1，R 2，R 3，R 4，R 8和A如说明书中所定义。

公开(公告)号：US4563472A

公开(公告)日：1986-01-07

申请号：US433011

申请日：1982-10-06

申请人： Shigeharu Inouye ,  Taro Niida ,  Keinosuke Miyauchi ,  Kuniomi Matsumoto ,  Eiichi Akita ,  Masao Koyama ,  Fumio Kai ,  Takashi Tsuruoka

发明人： Shigeharu Inouye ,  Taro Niida ,  Keinosuke Miyauchi ,  Kuniomi Matsumoto ,  Eiichi Akita ,  Masao Koyama ,  Fumio Kai ,  Takashi Tsuruoka

IPC分类号： A01N43/36 ,  A01N43/50 ,  A01N43/56 ,  A01N43/653 ,  A01N43/713 ,  C07D207/34 ,  C07D207/42 ,  C07D233/91 ,  C07D257/04 ,  C07D257/06 ,  C07D521/00 ,  A61K31/41

CPC分类号： C07D257/04 ,  A01N43/36 ,  A01N43/50 ,  A01N43/56 ,  A01N43/653 ,  A01N43/713 ,  C07D207/34 ,  C07D207/42 ,  C07D231/12 ,  C07D233/56 ,  C07D233/91 ,  C07D249/08 ,  C07D257/06

摘要： Triiodoallyl- or iodopropargyl-substituted heterocyclic aromatic compounds which can be prepared by reacting unsubstituted- or substituted nitrogen-containing heterocyclic compounds with corresponding iodine containing alcohol reactive derivatives in the presence of a base in an inert organic solvent. These new heterocyclic aromatic compounds have remarkable antibacterial and antifungal activities and are useful as antibacterial and antifungal agents in medicinal, agricultural and industrial fields.

摘要翻译： 三碘代烯丙基或碘炔丙基取代的杂环芳族化合物，其可以通过在碱存在下在惰性有机溶剂中使未取代或取代的含氮杂环化合物与相应的含碘醇反应性衍生物反应来制备。 这些新的杂环芳族化合物具有显着的抗菌和抗真菌活性，可用作药用，农业和工业领域的抗菌和抗真菌剂。